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Compound Detail

CHEMBL1088901

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CN(C)CCCC(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1

Basic Information

ChEMBL ID CHEMBL1088901
Phase Preclinical
Structure Type MOL
InChI Key QKNUBNZRMFTLIJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

428.3
MW (Da)
4.42
ALogP
5
HBA
2
HBD
70.2
PSA (Ų)
0.58
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H22BrN5O
MW 428.33
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.70

Activity Summary

IC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 6.72 6.72 190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 190.0 nM 6.72 Inhibition of EGFR Leu858Arg and Thr790Met mutant by HTRF assay 20222733

Literature References

PubMed DOI Target Context # Activities
20222733 10.1021/jm901877j ADMET 8
20222733 10.1021/jm901877j Unchecked 5
20222733 10.1021/jm901877j Epidermal growth factor receptor 3
20222733 10.1021/jm901877j Serine/threonine-protein kinase PLK1 1
20222733 10.1021/jm901877j Dual specificity tyrosine-phosphorylation-regulated kinase 3 1
20222733 10.1021/jm901877j Fibroblast growth factor receptor 1 1
20222733 10.1021/jm901877j Mitogen-activated protein kinase 14 1
20222733 10.1021/jm901877j Calcium/calmodulin-dependent protein kinase type 1 1
20222733 10.1021/jm901877j Mitogen-activated protein kinase kinase kinase kinase 2 1
20222733 10.1021/jm901877j Serine/threonine-protein kinase Chk2 1
20222733 10.1021/jm901877j Ephrin type-A receptor 2 1
20222733 10.1021/jm901877j Maternal embryonic leucine zipper kinase 1
20222733 10.1021/jm901877j MAP kinase-interacting serine/threonine-protein kinase 2 1
20222733 10.1021/jm901877j Serine/threonine-protein kinase D1 1
20222733 10.1021/jm901877j Proto-oncogene tyrosine-protein kinase Src 1
20222733 10.1021/jm901877j Misshapen-like kinase 1 1
20222733 10.1021/jm901877j Receptor-interacting serine/threonine-protein kinase 2 1
20222733 10.1021/jm901877j Ephrin type-B receptor 3 1
20222733 10.1021/jm901877j Tyrosine-protein kinase Yes 1
20222733 10.1021/jm901877j Tyrosine-protein kinase Lck 1

Data from ChEMBL 36 via Core Engine